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Exopeptidase Inhibitor
An exopeptidase inhibitor is a drug that inhibits one or more exopeptidase enzymes. Exopeptidases are one of two types of proteases (enzymes that break down proteins and peptides), the other being endopeptidases. Exopeptidases cleave peptide bonds of terminal amino acids, resulting in the release of a single amino acid or dipeptide from the peptide chain, whereas endoeptidases break non-terminal bonds (that is, they cut proteins/peptides into two chains). Some examples of exopeptidase inhibitors include amastatin, bestatin (ubenimex), puromycin, 1,10-phenanthroline, D-phenylalanine, ACE inhibitors, DPP-4 inhibitors, and exogenous MMP inhibitors like batimastat and marimastat. Various enkephalinase inhibitors, such as ketalorphan, spinorphin, and tynorphin, are mainly exopeptidase inhibitors. See also * Endopeptidase inhibitor An endopeptidase inhibitor is a drug that inhibits one or more endopeptidase enzymes. Endopeptidases are one of two types of proteases (enz ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Drug
A drug is any chemical substance that causes a change in an organism's physiology or psychology when consumed. Drugs are typically distinguished from food and substances that provide nutritional support. Consumption of drugs can be via insufflation (medicine), inhalation, drug injection, injection, smoking, ingestion, absorption (skin), absorption via a dermal patch, patch on the skin, suppository, or sublingual administration, dissolution under the tongue. In pharmacology, a drug is a chemical substance, typically of known structure, which, when administered to a living organism, produces a biological effect. A pharmaceutical drug, also called a medication or medicine, is a chemical substance used to pharmacotherapy, treat, cure, preventive healthcare, prevent, or medical diagnosis, diagnose a disease or to promote well-being. Traditionally drugs were obtained through extraction from medicinal plants, but more recently also by organic synthesis. Pharmaceutical drugs may be used ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
1,10-phenanthroline
1,10-Phenanthroline (phen) is a heterocyclic organic compound. It is a white solid that is soluble in organic solvents. The 1,10 refer to the location of the nitrogen atoms that replace CH's in the hydrocarbon called phenanthrene. Abbreviated "phen", it is used as a ligand in coordination chemistry, forming strong complexes with most metal ions.Luman, C.R. and Castellano, F.N. (2003) "Phenanthroline Ligands" in Comprehensive Coordination Chemistry II. Elsevier. . It is often sold as the monohydrate. Synthesis Phenanthroline may be prepared by two successive Skraup reactions of glycerol with ''o''-phenylenediamine, catalyzed by sulfuric acid, and an oxidizing agent, traditionally aqueous arsenic acid or nitrobenzene. Dehydration of glycerol gives acrolein which condenses with the amine followed by a cyclization. Coordination chemistry In terms of its coordination properties, phenanthroline is similar to 2,2'-bipyridine (bipy) with the advantage that the two nitrogen donor ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tynorphin
Tynorphin is a synthetic opioid peptide which is a potent and competitive inhibitor of the enkephalinase class of enzymes which break down the endogenous enkephalin peptides. It specifically inactivates dipeptidyl aminopeptidase III (DPP3) with very high efficacy, but also inhibits neutral endopeptidase (NEP), aminopeptidase N (APN), and angiotensin-converting enzyme (ACE) to a lesser extent. It has a pentapeptide structure with the amino acid sequence Val-Val-Tyr-Pro-Trp (VVYPW). Tynorphin was discovered in an attempt to develop an enkephalinase inhibitor of greater potency than spinorphin. See also * Enkephalinase inhibitor An enkephalinase inhibitor is a type of enzyme inhibitor which inhibits one or more members of the enkephalinase class of enzymes that break down the endogenous enkephalin opioid peptides. Examples include racecadotril, ubenimex (bestatin), RB-1 ... References {{Opioidergics Tryptamines Opioids Pentapeptides Propionic acids Pyrroli ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Spinorphin
Spinorphin is an endogenous, non-classical opioid peptide of the hemorphin family first isolated from the bovine spinal cord (hence the prefix ''spin''-) and acts as a regulator of the enkephalinases, a class of enzymes that break down endogenous the enkephalin peptides. It does so by inhibiting the enzymes aminopeptidase N (APN), dipeptidyl peptidase III (DPP3), angiotensin-converting enzyme (ACE), and neutral endopeptidase (NEP). Spinorphin is a heptapeptide and has the amino acid sequence Leu-Val-Val-Tyr-Pro-Trp-Thr (LVVYPWT). It has been observed to possess antinociceptive, antiallodynic, and anti-inflammatory properties. The mechanism of action of spinorphin has not been fully elucidated (i.e., how it acts to inhibit the enkephalinases), but it has been found to act as an antagonist of the P2X3 receptor, and as a weak partial agonist/antagonist of the FP1 receptor. See also * Enkephalinase inhibitor An enkephalinase inhibitor is a type of enzyme inhibitor which in ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ketalorphan
Kelatorphan is a drug which acts as a powerful and complete inhibitor of nearly all of the enzymes responsible for catabolism of the endogenous enkephalins, including neutral endopeptidase (NEP), dipeptidyl peptidase III (DPP3), aminopeptidase N (APN), and angiotensin-converting enzyme (ACE). In mice, with the intracerebroventricular co-administration of a 50 µg dose of kelatorphan (this route is necessary because kelatorphan is incapable of crossing the blood-brain-barrier) hence alongside exogenous etnkephalin ( ED50 approximately 10 ng), it potentiated the analgesic effects of the latter by 50,000 times. Kelatorphan also displays potent antinociceptive Nociception (also nocioception, from Latin ''nocere'' 'to harm or hurt') is the Somatosensory system, sensory nervous system's process of encoding Noxious stimulus, noxious stimuli. It deals with a series of events and processes required for an org ... effects alone, and does not depress respiration, although at ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Enkephalinase Inhibitor
An enkephalinase inhibitor is a type of enzyme inhibitor which inhibits one or more members of the enkephalinase class of enzymes that break down the endogenous enkephalin opioid peptides. Examples include racecadotril, ubenimex (bestatin), RB-101, and D-phenylalanine, as well as the endogenous opioid peptides opiorphin and spinorphin. It also includes RB-3007, Semax and Selank. Analgesic, anticraving, antidepressant, anxiolytic, and antidiarrheal effects are common properties of enkephalinase inhibitors. See also * Enkephalinase * Enkephalin An enkephalin is a pentapeptide involved in regulating nociception in the body. The enkephalins are termed endogenous ligands, as they are internally derived and bind to the body's opioid receptors. Discovered in 1975, two forms of enkephalin ... References Analgesics Antidiarrhoeals {{analgesic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Marimastat
Marimastat was a proposed antineoplastic drug developed by British Biotech. It acted as a broad-spectrum matrix metalloproteinase inhibitor A matrix metalloproteinase inhibitor (MMPI) inhibits matrix metalloproteinases. As they inhibit cell migration Cell migration is a central process in the development and maintenance of multicellular organisms. Tissue formation during embryonic d .... Marimastat performed poorly in clinical trials, and development was terminated. This may be, however, a result of targeting cancer at too late of a stage. This is supported by the fact that MMP inhibitors have more recently been shown in animal models to be more effective in earlier stages of cancers. (Effects of angiogenesis inhibitors on multistage carcinogenesis in mice. Science 284, 808-812. Bergers, G., Javaherian, K., Lo, K.-M., Folkman, J., and Hanahan, D. (1999)). See also * Batimastat References Experimental cancer drugs Hydroxamic acids Matrix metalloproteinase inhibito ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Batimastat
Batimastat (mnemonic: ''batty''-mustard) (INN/USAN, codenamed BB-94) is a drug that was invented by Laurie Hines of British Biotech (now Vernalis). It is an antimetastatic drug that belongs to the family of drugs called angiogenesis inhibitors. It acts as a matrix metalloproteinase inhibitor (MMPI) by mimicking natural MMPI peptides. Dan Lednicer wrote about this compound in book #6 of his organic drug synthesis series. Batimastat was the first MMPI that went into clinical trials. First results of a Phase I trial appeared in 1994. The drug reached Phase III but was never marketed; mainly because it couldn't be administered orally (as opposed to the newer and chemically similar MMPI marimastat), and injection into the peritoneum caused peritonitis Peritonitis is inflammation of the localized or generalized peritoneum, the lining of the inner wall of the abdomen and cover of the abdominal organs. Symptoms may include severe pain, swelling of the abdomen, fever, or weight loss. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Matrix Metalloproteinase Inhibitor
A matrix metalloproteinase inhibitor (MMPI) inhibits matrix metalloproteinases. As they inhibit cell migration Cell migration is a central process in the development and maintenance of multicellular organisms. Tissue formation during embryonic development, wound healing and immune responses all require the orchestrated movement of cells in particular dire ... they have antiangiogenic effects. They may be both endogenous and exogenous. The most notorious ''endogenous'' metalloproteinases are tissue inhibitors of metalloproteinases (TIMPs). There are also cartilage-derived angiogenesis inhibitors. ''Exogenous'' matrix metalloproteinase inhibitors were developed as anticancer drugs. Examples include: * Batimastat * Cipemastat * Ilomastat * Marimastat * MMI270 * Prinomastat * Rebimastat * Ro 28-2653 * Tanomastat Metalloproteinase inhibitors are found in numerous marine organisms, including fish, cephalopods, mollusks, algae, and bacteria. See also * Drug discovery and ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Exogenous
In a variety of contexts, exogeny or exogeneity () is the fact of an action or object originating externally. It contrasts with endogeneity or endogeny, the fact of being influenced within a system. Economics In an economic model, an exogenous change is one that comes from outside the model and is unexplained by the model. Such changes of an economic model from outside factors can include the influence of technology, in which this had previously been noted as an exogenous factor, but has rather been noted as a factor that can depict economic forces as a whole. In economic sociology, Project IDEA (Interdisciplinary Dimensions of Economic Analysis) gave notion to understanding the exogenous factors that play a role within economic theory. Developed from the International Social Science Council (ISSC) in the year of 1982, Project IDEA was founded to gather ideas from economists and sociologists in order to conceptualize what economic sociology incorporates, as they have sought ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
DPP-4 Inhibitor
Inhibitors of dipeptidyl peptidase 4 (DPP-4 inhibitors or gliptins) are a class of oral hypoglycemics that block the enzyme dipeptidyl peptidase-4 (DPP-4). They can be used to treat diabetes mellitus type 2. The first agent of the class – sitagliptin – was approved by the FDA in 2006. Glucagon increases blood glucose levels, and DPP-4 inhibitors reduce glucagon and blood glucose levels. The mechanism of DPP-4 inhibitors is to increase incretin levels (GLP-1 and GIP), which inhibit glucagon release, which in turn increases insulin secretion, decreases gastric emptying, and decreases blood glucose levels. A 2018 meta-analysis found no favorable effect of DPP-4 inhibitors on all-cause mortality, cardiovascular mortality, myocardial infarction or stroke in patients with type 2 diabetes. Examples Drugs belonging to this class are: * Sitagliptin (FDA approved 2006, marketed by Merck & Co. as Januvia) * Vildagliptin (EU approved 2007, marketed in the EU by Novartis as Galvus) * S ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
ACE Inhibitor
Angiotensin-converting-enzyme inhibitors (ACE inhibitors) are a class of medication used primarily for the treatment of hypertension, high blood pressure and heart failure. They work by causing relaxation of blood vessels as well as a decrease in blood volume, which leads to lower blood pressure and decreased oxygen demand from the heart. ACE inhibitors Enzyme inhibitor, inhibit the activity of angiotensin-converting enzyme, an important component of the renin–angiotensin system which converts angiotensin I to angiotensin II, and hydrolyses bradykinin. Therefore, ACE inhibitors decrease the formation of angiotensin II, a vasoconstrictor, and increase the level of bradykinin, a peptide vasodilator. This combination is synergistic in lowering blood pressure. As a result of inhibiting the ACE enzyme in the bradykinin system, the ACE inhibitor drugs allow for increased levels of bradykinin which would normally be degraded. Bradykinin produces prostaglandin. This mechanism can expl ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
